The Distribution of Drugs in the Central Nervous Sytem

  • A. V. Lorenzo
  • Reynold Spector
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 69)


The relative exclusion of many drugs from the central nervous system (CNS) is generally attributed to the blood-brain and blood- cerebrospinal fluid (CSF) barriers. In the past, this phenomenon was more or less interpreted as an impedance to the entry of drugs into the CNS. However, it is now apparent that numerous factors regulate the entry, as well as the distribution and final concentration of drugs within the CNS22. For instance, the rate of penetration from blood into the CNS is not only dependent on the plasma concentration, the physical-chemical properties7, 26, and the degree of binding of the drug to plasma proteins15, 47, but also on cerebral blood flow and the general permeability of cerebral blood vessels8, 20.Other factors beside the rate of penetration which affect the distribution of drugs within the CNS include regional vascularity, cerebral blood flow5, 36, the rate of diffusion through the interstitial spaces30 and CSF, uptake and metabolism within neuronal and glial elements, and the rate of efflux or diffusion from brain to CSF10 or to blood28, as well as efflux from CSF to blood29. The role and significance of factors which affect the penetration of molecules into the CNS will be dealt with in detail in the chapter by Dr. Oldendorf and will be alluded to by us only where necessary. The purpose of this chapter is to present the results of a series of studies conducted in our laboratories, as well as those of others, which lend support to the concept that the CSF plays an important role in the distribution and regulation of drugs within the CNS.


Salicylic Acid Choroid Plexus Lysergic Acid Efflux Mechanism Acta Physiol 
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Copyright information

© Plenum Press, New York 1976

Authors and Affiliations

  • A. V. Lorenzo
    • 1
  • Reynold Spector
    • 1
  1. 1.Departments of Pharmacology, Medicine, and NeurologyHarvard Medical SchoolBostonUSA

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